JP4611444B2 - ポリ(adp−リボース)ポリメラーゼ(parp)阻害剤としてのアミド置換インダゾール - Google Patents
ポリ(adp−リボース)ポリメラーゼ(parp)阻害剤としてのアミド置換インダゾール Download PDFInfo
- Publication number
- JP4611444B2 JP4611444B2 JP2009545240A JP2009545240A JP4611444B2 JP 4611444 B2 JP4611444 B2 JP 4611444B2 JP 2009545240 A JP2009545240 A JP 2009545240A JP 2009545240 A JP2009545240 A JP 2009545240A JP 4611444 B2 JP4611444 B2 JP 4611444B2
- Authority
- JP
- Japan
- Prior art keywords
- compound
- pharmaceutically acceptable
- acceptable salt
- indazole
- formula
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
- 0 *c1cc2c[n](C(C=C*3*=C)=CC=C3[Tl]=C)nc2c(*=C)c1 Chemical compound *c1cc2c[n](C(C=C*3*=C)=CC=C3[Tl]=C)nc2c(*=C)c1 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Virology (AREA)
- Diabetes (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Oncology (AREA)
- Urology & Nephrology (AREA)
- Molecular Biology (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Communicable Diseases (AREA)
- Rheumatology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Pulmonology (AREA)
- AIDS & HIV (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0700432.8A GB0700432D0 (en) | 2007-01-10 | 2007-01-10 | Therapeutic compounds |
| US92131007P | 2007-04-02 | 2007-04-02 | |
| PCT/GB2008/050018 WO2008084261A1 (en) | 2007-01-10 | 2008-01-08 | Amide substituted indazoles as poly(adp-ribose)polymerase (parp) inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010515715A JP2010515715A (ja) | 2010-05-13 |
| JP2010515715A5 JP2010515715A5 (enrdf_load_stackoverflow) | 2010-06-24 |
| JP4611444B2 true JP4611444B2 (ja) | 2011-01-12 |
Family
ID=39246752
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009545240A Active JP4611444B2 (ja) | 2007-01-10 | 2008-01-08 | ポリ(adp−リボース)ポリメラーゼ(parp)阻害剤としてのアミド置換インダゾール |
Country Status (31)
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2011509252A (ja) * | 2008-01-08 | 2011-03-24 | メルク シャープ エンド ドーム リミテッド | 2−{4−[(3s)−ピペリジン−3−イル]フェニル}−2h−インダゾール−7−カルボキサミドの薬学的に許容される塩 |
Families Citing this family (93)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7559282B2 (en) * | 2002-10-16 | 2009-07-14 | Robert Austin | Monorail sortation system |
| CA2615374A1 (en) * | 2005-07-18 | 2007-01-25 | Ernest Kun Kun | Treatment of cancer |
| AU2007232297B2 (en) * | 2006-04-03 | 2012-09-20 | Msd Italia S.R.L. | Amide substituted indazole and benzotriazole derivatives as poly(ADP-ribose)polymerase (PARP) inhibitors |
| CA2662517A1 (en) | 2006-09-05 | 2008-03-13 | Jerome Moore | Treatment of cancer |
| EP2061479A4 (en) * | 2006-09-05 | 2010-08-04 | Bipar Sciences Inc | FETTIC ACID SYNTHESIS INHIBITED BY PARP HEMMER AND TREATMENT PROCEDURES THEREWITH |
| BRPI0806542A2 (pt) | 2007-01-10 | 2014-04-22 | Hoffmann La Roche | Derivados de sulfonamida como inibidores de quimase |
| CA2705537A1 (en) | 2007-11-12 | 2009-05-22 | Bipar Sciences, Inc. | Treatment of breast cancer with a parp inhibitor alone or in combination with anti-tumor agents |
| WO2009085216A2 (en) | 2007-12-20 | 2009-07-09 | Squicor | Compositions and methods for detecting or elimninating senescent cells to diagnose or treat disease |
| US9101537B2 (en) | 2008-07-25 | 2015-08-11 | Reven Pharmaceuticals, Inc. | Compositions and methods for the prevention and treatment of cardiovascular diseases |
| MX2011008221A (es) * | 2009-02-04 | 2011-08-17 | Bipar Sciences Inc | Tratamiento de cancer de pulmon con un compuesto de nitrobenzamida en combinacion con un inhibidor de un factor de crecimieno. |
| WO2011058367A2 (en) | 2009-11-13 | 2011-05-19 | Astrazeneca Ab | Diagnostic test for predicting responsiveness to treatment with poly(adp-ribose) polymerase (parp) inhibitor |
| WO2011123795A1 (en) | 2010-04-02 | 2011-10-06 | Battelle Memorial Institute | Methods for associating or dissociating guest materials with a metal organic framework, systems for associating or dissociating guest materials within a series of metal organic frameworks, and gas separation assemblies |
| MX352481B (es) | 2010-07-22 | 2017-11-27 | Reven Pharmaceuticals Inc Star | Una solución de dipolo magnético estabilizado para tratar o aliviar enfermedades y mejorar el desempeño. |
| US20140189897A1 (en) | 2011-06-21 | 2014-07-03 | Mayo Foundation For Medical Education And Research | Transgenic animals capable of being induced to delete senescent cells |
| WO2013014038A1 (en) * | 2011-07-26 | 2013-01-31 | Nerviano Medical Sciences S.R.L. | 3-oxo-2,3-dihydro-1h-indazole-4-carboxamide derivatives as parp-1 inhibitors |
| KR101844880B1 (ko) | 2011-09-26 | 2018-04-03 | 닛토덴코 가부시키가이샤 | 증대된 태양에너지 수확 효율을 위한 높은 형광 및 광-안정한 발색단 |
| CN103415589B (zh) | 2011-10-05 | 2016-08-10 | 日东电工株式会社 | 具有提高日光采集效率的压敏粘附层的波长转换膜 |
| RU2014128010A (ru) | 2011-12-13 | 2016-02-10 | Бак Инститьют Фо Рисерч Он Эйджин | Способы улучшения средств консервативной терапии |
| US20150064137A1 (en) | 2012-04-17 | 2015-03-05 | Kythera Biopharmaceuticals, Inc. | Use of engineered viruses to specifically kill senescent cells |
| AR091731A1 (es) | 2012-07-19 | 2015-02-25 | Merck Sharp & Dohme | Antagonistas del receptor de mineralocorticoides |
| US9901081B2 (en) | 2012-08-23 | 2018-02-27 | Buck Institute For Research On Aging | Transgenic mouse for determining the role of senescent cells in cancer |
| US9901080B2 (en) | 2012-08-23 | 2018-02-27 | Buck Institute For Research On Aging | Transgenic mouse having a transgene that converts a prodrug into a cytotoxic compound in senescent cells |
| US9580407B2 (en) | 2012-12-07 | 2017-02-28 | Merck Sharp & Dohme Corp. | Regioselective N-2 arylation of indazoles |
| US9738915B2 (en) | 2012-12-07 | 2017-08-22 | Merck Sharp & Dohme Corp. | Biocatalytic transamination process |
| WO2015051766A1 (en) * | 2013-10-12 | 2015-04-16 | Betta Pharmaceuticals Co., Ltd | Amids substituted indazole derivativees as ploy (adp-ribose) polymerase inhibitors |
| SI3157566T1 (sl) | 2014-06-17 | 2019-08-30 | Vertex Pharmaceuticals Incorporated | Postopek za zdravljenje raka z uporabo kombinacije inhibitorjev CHK1 in ATR |
| WO2016138574A1 (en) | 2015-03-02 | 2016-09-09 | Sinai Health System | Homologous recombination factors |
| LT3277321T (lt) | 2015-04-01 | 2024-10-25 | Anaptysbio, Inc. | Antikūnai, nukreipti prieš t ląstelių imunoglobuliną ir mucino baltymą 3 (tim-3) |
| RU2768621C1 (ru) | 2015-09-30 | 2022-03-24 | Вертекс Фармасьютикалз Инкорпорейтед | Способ лечения рака с использованием комбинации повреждающих днк средств и ингибиторов atr |
| KR102750692B1 (ko) | 2015-12-14 | 2025-01-09 | 에프엠씨 코포레이션 | 헤테로사이클-치환된 비시클릭 아졸 살충제 |
| WO2017156350A1 (en) | 2016-03-09 | 2017-09-14 | K-Gen, Inc. | Methods of cancer treatment |
| WO2018005818A1 (en) | 2016-06-29 | 2018-01-04 | Tesaro, Inc. | Methods of treating ovarian cancer |
| PE20190403A1 (es) | 2016-07-29 | 2019-03-13 | Janssen Pharmaceutica Nv | Metodos para tratar el cancer de prostata |
| BR112019008859A2 (pt) | 2016-11-01 | 2019-07-09 | Anaptysbio Inc | anticorpos direcionados contra a morte programada 1 (pd-1) |
| MA46113A (fr) | 2016-11-01 | 2019-07-10 | Anaptysbio Inc | Anticorps dirigés contre l'immunoglobuline de lymphocyte t et la protéine 3 de mucine (tim-3) |
| CN108201537A (zh) * | 2016-12-16 | 2018-06-26 | 苏州苏融生物医药有限公司 | 一种尼拉帕尼缓控释药物组合物及其用途 |
| WO2018122168A1 (en) | 2016-12-29 | 2018-07-05 | Bayer Pharma Aktiengesellschaft | Combinations of bub1 kinase and parp inhibitors |
| EP3565844B8 (en) | 2017-01-09 | 2023-04-12 | Tesaro, Inc. | Methods of treating cancer with anti-pd-1 antibodies |
| SG10201913083SA (en) | 2017-01-09 | 2020-03-30 | Tesaro Inc | Methods of treating cancer with anti-tim-3 antibodies |
| WO2018136010A1 (en) | 2017-01-20 | 2018-07-26 | Aslan Pharmaceuticals Pte Ltd | Combination therapy |
| WO2018136009A1 (en) | 2017-01-20 | 2018-07-26 | Aslan Pharmaceuticals Pte Ltd | Combination therapy |
| EP3600314A1 (en) | 2017-03-27 | 2020-02-05 | Tesaro, Inc. | Niraparib compositions |
| JP7118347B2 (ja) * | 2017-04-04 | 2022-08-16 | コンビフォス カタリスツ インコーポレイテッド | 重水素化(s)2-(4-(ピペリジン-3-イル)フェニル)-2h-インダゾール-7-カルボキサミド |
| JOP20190244A1 (ar) | 2017-04-13 | 2019-10-13 | Janssen Pharmaceutica Nv | تركيبة علاجية لسرطان البروستاتا |
| ES2926255T3 (es) * | 2017-04-24 | 2022-10-24 | Tesaro Inc | Métodos de fabricación de niraparib |
| WO2018201096A1 (en) | 2017-04-27 | 2018-11-01 | Tesaro, Inc. | Antibody agents directed against lymphocyte activation gene-3 (lag-3) and uses thereof |
| AU2018264992A1 (en) | 2017-05-09 | 2019-12-05 | Merck Sharp & Dohme B.V. | Combination therapies for treating cancer |
| CA3063715A1 (en) | 2017-05-18 | 2018-11-22 | Tesaro, Inc. | Combination therapies for treating cancer |
| CN109081828B (zh) | 2017-06-14 | 2021-03-26 | 上海时莱生物技术有限公司 | 聚(adp-核糖)聚合酶抑制剂、制备方法及用途 |
| WO2018237296A1 (en) * | 2017-06-23 | 2018-12-27 | City Of Hope | Parg inhibitors and method of use thereof |
| EP3668857B1 (en) | 2017-08-14 | 2023-07-05 | Teva Pharmaceuticals International GmbH | Processes for the preparation of niraparib and intermediates thereof |
| BR112020006039A2 (pt) | 2017-09-26 | 2020-10-06 | Tesaro, Inc. | formulações de niraparibe |
| CA3076515A1 (en) | 2017-09-30 | 2019-04-04 | Tesaro, Inc. | Combination therapies for treating cancer |
| SG11202002499TA (en) | 2017-10-06 | 2020-04-29 | Tesaro Inc | Combination therapies and uses thereof |
| WO2019083457A1 (en) | 2017-10-25 | 2019-05-02 | Aslan Pharmaceuticals Pte Ltd | VARLITINIB FOR USE IN THE TREATMENT OF CANCER IN A PATIENT IDENTIFIED AS MUTATION OF THE BETA-CATENIN PATHWAY |
| WO2019083458A1 (en) | 2017-10-25 | 2019-05-02 | Aslan Pharmaceuticals Pte Ltd | VARLITINIB FOR THE TREATMENT OF CANCER TO REDUCE HYPOXIA |
| WO2019083456A1 (en) | 2017-10-25 | 2019-05-02 | Aslan Pharmaceuticals Pte Ltd | VARLITINIB FOR USE IN THE TREATMENT OF CANCER FOR NORMALIZING ANGIOGENESIS IN A CANCER MASS |
| WO2019083455A1 (en) | 2017-10-25 | 2019-05-02 | Aslan Pharmaceuticals Pte Ltd | VARLITINIB FOR USE IN THE TREATMENT OF CANCER IN A PATIENT IDENTIFIED AS PRESENTING HER1, HER2 AND / OR HER3-ACTIVATED HERC-RECEPTOR CANCER CELLS |
| CN111565709A (zh) | 2017-12-07 | 2020-08-21 | 雷文知识产权控股有限公司 | 治疗代谢病症的组合物和方法 |
| TW201929902A (zh) | 2017-12-27 | 2019-08-01 | 美商提薩羅有限公司 | 治療癌症之方法 |
| EP3735297A1 (en) | 2018-01-05 | 2020-11-11 | Cybrexa 1, Inc. | Compounds, compositions, and methods for treatment of diseases involving acidic or hypoxic diseased tissues |
| CN111918667A (zh) | 2018-02-05 | 2020-11-10 | 特沙诺有限公司 | 儿科尼拉帕尼配制剂和儿科治疗方法 |
| WO2019196812A1 (zh) * | 2018-04-09 | 2019-10-17 | 上海科技大学 | 蛋白降解靶向化合物、其抗肿瘤应用、其中间体及中间体应用 |
| TWI852940B (zh) | 2018-09-04 | 2024-08-21 | 美商泰沙羅公司 | 治療癌症之方法 |
| CN113330007A (zh) | 2018-10-03 | 2021-08-31 | 特沙诺有限公司 | 尼拉帕利游离碱的晶体形式 |
| WO2020072860A1 (en) | 2018-10-05 | 2020-04-09 | Johnson Matthey Public Limited Company | Niraparib solid state form |
| JP2022510501A (ja) | 2018-10-30 | 2022-01-26 | リペア セラピューティクス インコーポレイテッド | 化合物、医薬組成物、ならびに化合物の調製方法及びatrキナーゼ阻害剤としてのその使用方法 |
| WO2020225753A2 (en) | 2019-05-06 | 2020-11-12 | Tesaro, Inc. | Methods for characterizing and treating a cancer type using cancer images |
| CN110156751B (zh) * | 2019-05-28 | 2022-01-18 | 江苏食品药品职业技术学院 | 一种制备尼拉帕尼及其中间体的新方法 |
| AR120059A1 (es) * | 2019-06-12 | 2022-02-02 | Reven Ip Holdco Llc | Métodos y composiciones para mejorar resultados de pacientes con cáncer |
| JP7675060B2 (ja) | 2019-07-10 | 2025-05-12 | サイブレクサ 3,インコーポレイテッド | 治療薬としての微小管標的化剤のペプチドコンジュゲート |
| US11634508B2 (en) | 2019-07-10 | 2023-04-25 | Cybrexa 2, Inc. | Peptide conjugates of cytotoxins as therapeutics |
| PH12022553029A1 (en) * | 2020-05-08 | 2024-05-13 | Janssen Pharmaceutica Nv | Treatments of prostate cancer with combinations of abiraterone acetate and niraparib |
| PE20240119A1 (es) | 2021-01-08 | 2024-01-22 | Cybrexa 2 Inc | Proceso para preparar un resto enlazador de conjugados |
| WO2022155172A1 (en) | 2021-01-13 | 2022-07-21 | Cybrexa 3, Inc. | Peptide conjugates of therapeutics |
| US20240197730A1 (en) * | 2021-04-09 | 2024-06-20 | Cardiff Oncology, Inc. | Cancer treatment using parp inhibitors and plk1 inhibitors |
| MX2024000949A (es) | 2021-07-19 | 2024-02-08 | Janssen Pharmaceutica Nv | Tratamiento de cancer de prostata metastasico resistente a la castracion con niraparib. |
| MX2024009626A (es) | 2022-02-04 | 2024-08-09 | Janssen Pharmaceutica Nv | Niraparib y acetato de abiraterona mas prednisona para mejorar los resultados clinicos en pacientes con cancer de prostata resistente a la castracion metastasico y alteraciones del hrr. |
| CN119156216A (zh) | 2022-02-15 | 2024-12-17 | 特沙诺有限公司 | 尼拉帕尼用于治疗脑癌的用途 |
| WO2023201338A1 (en) | 2022-04-15 | 2023-10-19 | Ideaya Biosciences, Inc. | Combination therapy comprising a mat2a inhibitor and a parp inhibitor |
| EP4532493A1 (en) | 2022-06-01 | 2025-04-09 | Ideaya Biosciences, Inc. | Thiadiazolyl derivatives as dna polymerase theta inhibitors and uses thereof |
| WO2024054898A1 (en) * | 2022-09-08 | 2024-03-14 | Cardiff Oncology, Inc. | Onvansertib and parp inhibitor combination |
| IL319474A (en) | 2022-09-11 | 2025-05-01 | Cardiff Oncology Inc | PLK1 inhibitor combined with anti-angiogenesis for the treatment of metastatic cancer |
| WO2024142096A1 (en) * | 2022-12-29 | 2024-07-04 | Dr. Reddy’S Laboratories Limited | Process for preparation of niraparib tosylate and its intermediates |
| WO2024229406A1 (en) | 2023-05-04 | 2024-11-07 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| WO2024238587A1 (en) | 2023-05-17 | 2024-11-21 | Tesaro, Inc. | Novel use of an inhibior of the a poly-adp ribose polymerase (parp) in the treatment of cancer |
| WO2025017711A1 (en) * | 2023-07-20 | 2025-01-23 | Natco Pharma Limited | An improved process for the preparation of niraparib tosylate monohydrate |
| WO2025027138A1 (en) | 2023-08-02 | 2025-02-06 | Janssen Pharmaceutica Nv | Combination of niraparib and abiraterone for use in the treatment of metastatic castration-resistant prostate cancer |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| TW202530228A (zh) | 2023-10-12 | 2025-08-01 | 美商銳新醫藥公司 | Ras抑制劑 |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025217307A1 (en) | 2024-04-09 | 2025-10-16 | Revolution Medicines, Inc. | Methods for predicting response to a ras(on) inhibitor and combination therapies |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
Family Cites Families (345)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3126375A (en) | 1964-03-24 | Chioacyl | ||
| US2789118A (en) | 1956-03-30 | 1957-04-16 | American Cyanamid Co | 16-alpha oxy-belta1, 4-pregnadienes |
| US2990401A (en) | 1958-06-18 | 1961-06-27 | American Cyanamid Co | 11-substituted 16alpha, 17alpha-substituted methylenedioxy steroids |
| US3048581A (en) | 1960-04-25 | 1962-08-07 | Olin Mathieson | Acetals and ketals of 16, 17-dihydroxy steroids |
| US3749712A (en) | 1970-09-25 | 1973-07-31 | Sigma Tau Ind Farmaceuti | Triamcinolone acetonide esters and process for their preparation |
| SE378110B (enrdf_load_stackoverflow) | 1972-05-19 | 1975-08-18 | Bofors Ab | |
| US3996359A (en) | 1972-05-19 | 1976-12-07 | Ab Bofors | Novel stereoisomeric component A of stereoisomeric mixtures of 2'-unsymmetrical 16,17-methylenedioxy steroid 21-acylates, compositions thereof, and method of treating therewith |
| SE378109B (enrdf_load_stackoverflow) | 1972-05-19 | 1975-08-18 | Bofors Ab | |
| US4294926A (en) | 1979-06-15 | 1981-10-13 | Merck & Co., Inc. | Hypocholesteremic fermentation products and process of preparation |
| US4319039A (en) | 1979-06-15 | 1982-03-09 | Merck & Co., Inc. | Preparation of ammonium salt of hypocholesteremic fermentation product |
| US4231938A (en) | 1979-06-15 | 1980-11-04 | Merck & Co., Inc. | Hypocholesteremic fermentation products and process of preparation |
| US4444784A (en) | 1980-08-05 | 1984-04-24 | Merck & Co., Inc. | Antihypercholesterolemic compounds |
| MX7065E (es) | 1980-06-06 | 1987-04-10 | Sankyo Co | Un procedimiento microbiologico para preparar derivados de ml-236b |
| JPS5889191A (ja) | 1981-11-20 | 1983-05-27 | Sankyo Co Ltd | 3−ヒドロキシ−ml−236b誘導体の製造法 |
| US5354772A (en) | 1982-11-22 | 1994-10-11 | Sandoz Pharm. Corp. | Indole analogs of mevalonolactone and derivatives thereof |
| US4911165A (en) | 1983-01-12 | 1990-03-27 | Ethicon, Inc. | Pliabilized polypropylene surgical filaments |
| US5041653A (en) | 1985-05-03 | 1991-08-20 | Sri International | Substituted benzamide radiosensitizers |
| US5032617A (en) | 1985-05-03 | 1991-07-16 | Sri International | Substituted benzamide radiosensitizers |
| US5215738A (en) | 1985-05-03 | 1993-06-01 | Sri International | Benzamide and nicotinamide radiosensitizers |
| US4681893A (en) | 1986-05-30 | 1987-07-21 | Warner-Lambert Company | Trans-6-[2-(3- or 4-carboxamido-substituted pyrrol-1-yl)alkyl]-4-hydroxypyran-2-one inhibitors of cholesterol synthesis |
| US4885314A (en) | 1987-06-29 | 1989-12-05 | Merck & Co., Inc. | Novel HMG-CoA reductase inhibitors |
| US4782084A (en) | 1987-06-29 | 1988-11-01 | Merck & Co., Inc. | HMG-COA reductase inhibitors |
| US4820850A (en) | 1987-07-10 | 1989-04-11 | Merck & Co., Inc. | Process for α-C-alkylation of the 8-acyl group on mevinolin and analogs thereof |
| US5180589A (en) | 1988-03-31 | 1993-01-19 | E. R. Squibb & Sons, Inc. | Pravastatin pharmaceuatical compositions having good stability |
| US5030447A (en) | 1988-03-31 | 1991-07-09 | E. R. Squibb & Sons, Inc. | Pharmaceutical compositions having good stability |
| US4916239A (en) | 1988-07-19 | 1990-04-10 | Merck & Co., Inc. | Process for the lactonization of mevinic acids and analogs thereof |
| EP0360390A1 (en) | 1988-07-25 | 1990-03-28 | Glaxo Group Limited | Spirolactam derivatives |
| US5290946A (en) | 1988-10-13 | 1994-03-01 | Sandoz Ltd. | Processes for the synthesis of 3-(substituted indolyl-2-yl)propenaldehydes |
| US5118853A (en) | 1988-10-13 | 1992-06-02 | Sandoz Ltd. | Processes for the synthesis of 3-disubstituted aminoacroleins |
| WO1990005525A1 (en) | 1988-11-23 | 1990-05-31 | Pfizer Inc. | Quinuclidine derivatives as substance p antagonists |
| US4929437A (en) | 1989-02-02 | 1990-05-29 | Merck & Co., Inc. | Coenzyme Q10 with HMG-CoA reductase inhibitors |
| US5164372A (en) | 1989-04-28 | 1992-11-17 | Fujisawa Pharmaceutical Company, Ltd. | Peptide compounds having substance p antagonism, processes for preparation thereof and pharmaceutical composition comprising the same |
| US5189164A (en) | 1989-05-22 | 1993-02-23 | Sandoz Ltd. | Processes for the synthesis of syn-(E)-3,5-dihydroxy-7-substituted hept-6-enoic and heptanoic acids and derivatives and intermediates thereof |
| FI94339C (fi) | 1989-07-21 | 1995-08-25 | Warner Lambert Co | Menetelmä farmaseuttisesti käyttökelpoisen /R-(R*,R*)/-2-(4-fluorifenyyli)- , -dihydroksi-5-(1-metyylietyyli)-3-fenyyli-4-/(fenyyliamino)karbonyyli/-1H-pyrroli-1-heptaanihapon ja sen farmaseuttisesti hyväksyttävien suolojen valmistamiseksi |
| PH27357A (en) | 1989-09-22 | 1993-06-21 | Fujisawa Pharmaceutical Co | Pyrazole derivatives and pharmaceutical compositions comprising the same |
| IE903957A1 (en) | 1989-11-06 | 1991-05-08 | Sanofi Sa | Aromatic amine compounds, their method of preparation and¹pharmaceutical compositions in which they are present |
| FR2654726B1 (fr) | 1989-11-23 | 1992-02-14 | Rhone Poulenc Sante | Nouveaux derives de l'isoindolone et leur preparation. |
| FR2654725B1 (fr) | 1989-11-23 | 1992-02-14 | Rhone Poulenc Sante | Nouveaux derives de l'isoindolone, leur preparation et les compositions pharmaceutiques qui les contiennent. |
| GB8929070D0 (en) | 1989-12-22 | 1990-02-28 | Fujisawa Pharmaceutical Co | Peptide compounds,processes for preparation thereof and pharmaceutical composition comprising the same |
| US5232929A (en) | 1990-11-28 | 1993-08-03 | Pfizer Inc. | 3-aminopiperidine derivatives and related nitrogen containing heterocycles and pharmaceutical compositions and use |
| WO1991009844A1 (en) | 1990-01-04 | 1991-07-11 | Pfizer Inc. | Substance p antagonists |
| WO1991012266A1 (fr) | 1990-02-15 | 1991-08-22 | Fujisawa Pharmaceutical Co., Ltd. | Compose peptidique |
| US5420245A (en) | 1990-04-18 | 1995-05-30 | Board Of Regents, The University Of Texas | Tetrapeptide-based inhibitors of farnesyl transferase |
| GB9011833D0 (en) | 1990-05-25 | 1990-07-18 | Collins Mary K L | Inhibition of viral infection |
| HUT62891A (en) | 1990-06-01 | 1993-06-28 | Pfizer | Process for producing 3-amino-2-arylquinuclidine compounds and pharmaceuticql composition comprising such compounds |
| PL167568B1 (pl) | 1990-07-23 | 1995-09-30 | Pfizer | Sposób wytwarzania nowych pochodnych chinuklidyny PL PL |
| ES2071334T3 (es) | 1990-09-28 | 1995-06-16 | Pfizer | Analogos de anillos fusionados de nitrogeno conteniendo heterociclos no aromaticos. |
| GB9023116D0 (en) | 1990-10-24 | 1990-12-05 | Fujisawa Pharmaceutical Co | Peptide compounds,processes for preparation thereof and pharmaceutical composition comprising the same |
| EP0498069B1 (en) | 1990-12-21 | 1995-10-25 | Fujisawa Pharmaceutical Co., Ltd. | New use of peptide derivative |
| JPH0733385B2 (ja) | 1991-01-10 | 1995-04-12 | フアイザー・インコーポレイテツド | 物質pの拮抗薬としてのn−アルキルキヌクリジニウム塩 |
| DE69220258T2 (de) | 1991-02-11 | 1997-12-18 | Merck Sharp & Dohme | Azabicyclische Verbindungen, diese enthaltende pharmazeutische Zubereitungen und ihre therapeutische Verwendung |
| DK0573522T3 (da) | 1991-03-01 | 1995-03-06 | Pfizer | 1-Azabicyclo(3,2,2)nonan-3-aminderivater |
| US5747469A (en) | 1991-03-06 | 1998-05-05 | Board Of Regents, The University Of Texas System | Methods and compositions comprising DNA damaging agents and p53 |
| WO1992017449A1 (en) | 1991-03-26 | 1992-10-15 | Pfizer Inc. | Stereoselective preparation of substituted piperidines |
| FR2677361A1 (fr) | 1991-06-04 | 1992-12-11 | Adir | Nouveaux peptides et pseudopeptides, derives de tachykinines, leur procede de preparation et les compositions pharmaceutiques qui les contiennent. |
| FR2676055B1 (fr) | 1991-05-03 | 1993-09-03 | Sanofi Elf | Composes polycycliques amines et leurs enantiomeres, procede pour leur preparation et compositions pharmaceutiques les contenant. |
| FR2676053B1 (fr) | 1991-05-03 | 1993-08-27 | Sanofi Elf | Nouveaux composes dialkylenepiperidino et leurs enantiomeres, procede pour leur preparation et compositions pharmaceutiques les contenant. |
| FR2676447B1 (fr) | 1991-05-17 | 1993-08-06 | Rhone Poulenc Rorer Sa | Nouveaux derives du thiopyranopyrrole et leur preparation. |
| FR2676446B1 (fr) | 1991-05-17 | 1993-08-06 | Rhone Poulenc Rorer Sa | Nouveaux derives du thiopyranopyrrole, leur preparation et les compositions pharmaceutiques qui les contiennent. |
| FR2676443B1 (fr) | 1991-05-17 | 1993-08-06 | Rhone Poulenc Rorer Sa | Nouveaux derives de perhydroisoindole et leur preparation. |
| FR2676442B1 (fr) | 1991-05-17 | 1993-08-06 | Rhone Poulenc Rorer Sa | Nouveau derives de perhydroisoindole, leur preparation et les compositions pharmaceutiques qui les contiennent. |
| WO1992020661A1 (en) | 1991-05-22 | 1992-11-26 | Merck & Co., Inc. | N, n-diacylpiperazines |
| ATE211743T1 (de) | 1991-05-22 | 2002-01-15 | Pfizer | Substituierte 3-aminochinuclidine |
| CZ281403B6 (cs) | 1991-05-31 | 1996-09-11 | Pfizer Inc. | Chinuklidinové deriváty, způsob jejich přípravy a použití. |
| GB9113219D0 (en) | 1991-06-19 | 1991-08-07 | Fujisawa Pharmaceutical Co | Peptide compound,processes for preparation thereof and pharmaceutical composition comprising the same |
| CA2109613C (en) | 1991-06-20 | 1996-11-19 | John Adams Lowe Iii | Fluoroalkoxybenzylamino derivatives of nitrogen containing heterocycles |
| TW202432B (enrdf_load_stackoverflow) | 1991-06-21 | 1993-03-21 | Pfizer | |
| US5288730A (en) | 1991-06-24 | 1994-02-22 | Merck Sharp & Dohme Limited | Azabicyclic compounds, pharmaceutical compositions containing them and their use in therapy |
| CA2110514A1 (en) | 1991-07-05 | 1993-01-21 | Raymond Baker | Aromatic compounds, pharmaceutical compositions containing them and their use in therapy |
| EP0536817A1 (en) | 1991-07-05 | 1993-04-14 | MERCK SHARP & DOHME LTD. | Azabicyclic compounds as tachykinin antagonists |
| IE72090B1 (en) | 1991-07-05 | 1997-03-12 | Merck Sharp & Dohme | Aromatic compounds pharmaceutical compositions containing them and their use in therapy |
| US5495047A (en) | 1991-07-10 | 1996-02-27 | Merck, Sharp & Dohme (Ltd.) | Fused tricyclic compounds, pharmaceutical compositions containing them and their use in therapy |
| EP0593615B1 (en) | 1991-07-10 | 1996-01-31 | MERCK SHARP & DOHME LTD. | Aromatic compounds, compositions containing them and their use in therapy |
| MY110227A (en) | 1991-08-12 | 1998-03-31 | Ciba Geigy Ag | 1-acylpiperindine compounds. |
| JPH06510034A (ja) | 1991-08-20 | 1994-11-10 | メルク シヤープ エンド ドーム リミテツド | アザ環式化合物、それらの製造方法、及びそれらを含む医薬組成物 |
| EP1082959A1 (en) | 1991-09-20 | 2001-03-14 | Glaxo Group Limited | NK1 Antagonists for the treatment of depression |
| CZ59394A3 (en) | 1991-09-26 | 1994-11-16 | Pfizer | Condensed tricyclic heterocycles containing nitrogen as antagonists of p substance receptor, process of their preparation, intermediates, pharmaceutical preparations in which they are comprised and use |
| US5652260A (en) | 1991-10-22 | 1997-07-29 | Octamer, Inc. | Adenosine diphosphoribose polymerase binding nitroso aromatic compound useful as retroviral inactivating agents, anti-retroviral agents and anti-tumor agents |
| WO1993009116A1 (fr) | 1991-11-07 | 1993-05-13 | Yoshitomi Pharmaceutical Industries, Ltd. | Compose a base de quinuclidine et utilisation dudit compose en medecine |
| HUT70741A (en) | 1991-11-12 | 1995-10-30 | Pfizer | Acyclic ethylenediamine derivatives as substance p receptor antagonists |
| CA2083891A1 (en) | 1991-12-03 | 1993-06-04 | Angus Murray Macleod | Heterocyclic compounds, compositions containing them and their use in therapy |
| HU9203780D0 (en) | 1991-12-12 | 1993-03-29 | Sandoz Ag | Stabilized pharmaceutical products of hmg-coa reductase inhibitor and method for producing them |
| GB9200535D0 (en) | 1992-01-10 | 1992-02-26 | Fujisawa Pharmaceutical Co | New compound |
| GB9201179D0 (en) | 1992-01-21 | 1992-03-11 | Glaxo Group Ltd | Chemical compounds |
| US5328927A (en) | 1992-03-03 | 1994-07-12 | Merck Sharpe & Dohme, Ltd. | Hetercyclic compounds, processes for their preparation and pharmaceutical compositions containing them |
| JP2656702B2 (ja) | 1992-03-23 | 1997-09-24 | ファイザー製薬株式会社 | ペプチド性キヌクリジン |
| FR2689888B1 (fr) | 1992-04-10 | 1994-06-10 | Rhone Poulenc Rorer Sa | Nouveaux derives de perhydroisoindole, leur preparation et les compositions pharmaceutiques qui les contiennent. |
| JPH07505648A (ja) | 1992-04-15 | 1995-06-22 | メルク シヤープ エンド ドーム リミテツド | アザサイクリック化合物 |
| GB2266529A (en) | 1992-05-01 | 1993-11-03 | Merck Sharp & Dohme | Tetrahydroisoquinoline derivatives |
| CA2134964C (en) | 1992-05-18 | 1997-12-30 | Manoj C. Desai | Bridged aza-bicyclic derivatives as substance p antagonists |
| GB9211193D0 (en) | 1992-05-27 | 1992-07-08 | Merck Sharp & Dohme | Therapeutic agents |
| US5637699A (en) | 1992-06-29 | 1997-06-10 | Merck & Co., Inc. | Process for preparing morpholine tachykinin receptor antagonists |
| US5719147A (en) | 1992-06-29 | 1998-02-17 | Merck & Co., Inc. | Morpholine and thiomorpholine tachykinin receptor antagonists |
| IL106142A (en) | 1992-06-29 | 1997-03-18 | Merck & Co Inc | Morpholine and thiomorpholine tachykinin receptor antagonists, their preparation and pharmaceutical compositions containing them |
| WO1994001402A1 (en) | 1992-07-13 | 1994-01-20 | Merck Sharp & Dohme Limited | Heterocyclic amide derivatives as tachykinin derivatives |
| EP0786522A2 (en) | 1992-07-17 | 1997-07-30 | Ribozyme Pharmaceuticals, Inc. | Enzymatic RNA molecules for treatment of stenotic conditions |
| GB2268931A (en) | 1992-07-22 | 1994-01-26 | Merck Sharp & Dohme | Azabicyclic tachykinin-receptor antagonists |
| AU675447B2 (en) | 1992-07-28 | 1997-02-06 | Merck Sharp & Dohme Limited | Carboxamidomethyl piperidine and analogues |
| GB2269170A (en) | 1992-07-29 | 1994-02-02 | Merck Sharp & Dohme | Azatricyclic tachykinin antagonists |
| AU4718093A (en) | 1992-07-31 | 1994-03-03 | Merck Sharp & Dohme Limited | Substituted amines as tachykinin receptor antagonists |
| AU4396193A (en) | 1992-08-04 | 1994-03-03 | Pfizer Inc. | 3-benzylamino-2-phenyl-piperidine derivatives as substance p receptor antagonists |
| GB9216911D0 (en) | 1992-08-10 | 1992-09-23 | Merck Sharp & Dohme | Therapeutic agents |
| DK0655055T3 (da) | 1992-08-13 | 2001-01-02 | Warner Lambert Co | Tachykininantagonister |
| JP2909214B2 (ja) | 1992-08-19 | 1999-06-23 | フアイザー・インコーポレイテツド | 置換ベンジルアミノ窒素含有非芳香族複素環化合物 |
| US5387595A (en) | 1992-08-26 | 1995-02-07 | Merck & Co., Inc. | Alicyclic compounds as tachykinin receptor antagonists |
| DE69315920T2 (de) | 1992-09-04 | 1998-06-10 | Takeda Chemical Industries Ltd | Kondensierte heterozyklische Verbindungen, deren Herstellung und Verwendung |
| AU4973693A (en) | 1992-09-10 | 1994-03-29 | Merck Sharp & Dohme Limited | Alcohols and ethers with aromatic substituents as tachykinin-antagonists |
| GB9220286D0 (en) | 1992-09-25 | 1992-11-11 | Merck Sharp & Dohme | Therapeutic agents |
| JP2656699B2 (ja) | 1992-10-21 | 1997-09-24 | ファイザー製薬株式会社 | 置換ベンジルアミノキヌクリジン |
| GB9222262D0 (en) | 1992-10-23 | 1992-12-09 | Merck Sharp & Dohme | Therapeutic agents |
| GB9222486D0 (en) | 1992-10-26 | 1992-12-09 | Merck Sharp & Dohme | Therapeutic agents |
| US5620989A (en) | 1992-10-28 | 1997-04-15 | Merck Sharp & Dohme Limited | 4-Arylmethyloxymethyl piperidines as tachykinin antagonsits |
| JP2656700B2 (ja) | 1992-10-28 | 1997-09-24 | ファイザー製薬株式会社 | 置換キヌクリジン誘導体 |
| WO1994010167A1 (en) | 1992-10-30 | 1994-05-11 | Merck Sharp & Dohme Limited | Tachykinin antagonists |
| JP2668164B2 (ja) | 1992-11-12 | 1997-10-27 | ファイザー・インク. | P物質拮抗薬としてのキヌクリジン誘導体 |
| US5261188A (en) | 1992-11-23 | 1993-11-16 | The Standard Products Company | Belt weatherstrip with bulb |
| EP0675886B1 (en) | 1992-12-10 | 2000-07-05 | Pfizer Inc. | Aminomethylene substituted non-aromatic heterocycles and use as substance p antagonists |
| US5604260A (en) | 1992-12-11 | 1997-02-18 | Merck Frosst Canada Inc. | 5-methanesulfonamido-1-indanones as an inhibitor of cyclooxygenase-2 |
| JPH08504435A (ja) | 1992-12-14 | 1996-05-14 | メルク シヤープ エンド ドーム リミテツド | タキキニン受容体拮抗剤としての4−アミノメチル/チオメチル/スルホニルメチル−4−フェニルピペリジン |
| GB9226581D0 (en) | 1992-12-21 | 1993-02-17 | Merck Sharp & Dohme | Therapeutic agents |
| CA2111902A1 (en) | 1992-12-21 | 1994-06-22 | Jack Beuford Campbell | Antitumor compositions and methods of treatment |
| GB9300051D0 (en) | 1993-01-04 | 1993-03-03 | Merck Sharp & Dohme | Therapeutic agents |
| DK0679157T3 (da) | 1993-01-15 | 1998-07-27 | Searle & Co | Nye 3,4-diarylthiophener og analoge deraf til anvendelse som antiinflammatoriske midler |
| US5466689A (en) | 1993-02-08 | 1995-11-14 | Takeda Chemical Industries, Ltd. | Morpholine derivatives and their use |
| AU679207B2 (en) | 1993-02-18 | 1997-06-26 | Merck Sharp & Dohme Limited | Azacyclic compounds, compositions containing them and their use as tachykinin antagonists |
| US5674889A (en) | 1993-02-22 | 1997-10-07 | Merck, Sharp & Dohme, Ltd. | Aromatic compounds, compositions containing them and their use in therapy |
| WO1994019357A1 (en) | 1993-02-23 | 1994-09-01 | Merrell Dow Pharmaceuticals Inc. | Farnesyl:protein transferase inhibitors as anticancer agents |
| US5298627A (en) | 1993-03-03 | 1994-03-29 | Warner-Lambert Company | Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis |
| WO1994020500A1 (en) | 1993-03-04 | 1994-09-15 | Pfizer Inc. | Spiroazacyclic derivatives as substance p antagonists |
| US5409944A (en) | 1993-03-12 | 1995-04-25 | Merck Frosst Canada, Inc. | Alkanesulfonamido-1-indanone derivatives as inhibitors of cyclooxygenase |
| CA2118985A1 (en) | 1993-04-02 | 1994-10-03 | Dinesh V. Patel | Heterocyclic inhibitors of farnesyl protein transferase |
| US5496833A (en) | 1993-04-13 | 1996-03-05 | Merck Sharp & Dohme Limited | Piperidine tachykinin receptor antagonists |
| WO1994026735A1 (en) | 1993-05-06 | 1994-11-24 | Merrell Dow Pharmaceuticals Inc. | Substituted pyrrolidin-3-yl-alkyl-piperidines useful as tachykinin antagonists |
| JPH09500615A (ja) | 1993-05-14 | 1997-01-21 | ジェネンテク,インコーポレイテッド | Ras−ファルネシル転移酵素阻害剤 |
| US5602098A (en) | 1993-05-18 | 1997-02-11 | University Of Pittsburgh | Inhibition of farnesyltransferase |
| IL109646A0 (en) | 1993-05-19 | 1994-08-26 | Pfizer | Heteroatom substituted alkyl benzylamino-quinuclidines |
| US5380738A (en) | 1993-05-21 | 1995-01-10 | Monsanto Company | 2-substituted oxazoles further substituted by 4-fluorophenyl and 4-methylsulfonylphenyl as antiinflammatory agents |
| EP0702681A1 (en) | 1993-06-07 | 1996-03-27 | Merck & Co. Inc. | Spiro-substituted azacycles as neurokinin antagonists |
| US5436265A (en) | 1993-11-12 | 1995-07-25 | Merck Frosst Canada, Inc. | 1-aroyl-3-indolyl alkanoic acids and derivatives thereof useful as anti-inflammatory agents |
| US5474995A (en) | 1993-06-24 | 1995-12-12 | Merck Frosst Canada, Inc. | Phenyl heterocycles as cox-2 inhibitors |
| GB9602877D0 (en) | 1996-02-13 | 1996-04-10 | Merck Frosst Canada Inc | 3,4-Diaryl-2-hydroxy-2,5- dihydrofurans as prodrugs to cox-2 inhibitors |
| EP0634402A1 (en) | 1993-07-14 | 1995-01-18 | Takeda Chemical Industries, Ltd. | Isochinolinone derivatives, their production and use |
| CA2167198C (en) | 1993-07-15 | 1999-03-16 | Kunio Satake | Benzylaminoquinuclidines |
| TW365603B (en) | 1993-07-30 | 1999-08-01 | Rhone Poulenc Rorer Sa | Novel perhydroisoindole derivatives, their preparation and pharmaceutical compositions which contain them |
| GB9315808D0 (en) | 1993-07-30 | 1993-09-15 | Merck Sharp & Dohme | Therapeutic agents |
| GB9317987D0 (en) | 1993-08-26 | 1993-10-13 | Glaxo Group Ltd | Chemical compounds |
| ATE265432T1 (de) | 1993-09-17 | 2004-05-15 | Pfizer | 3-amino-5-carboxy-substituierte piperidine und 3- amino-4-carboxy-substituierte pyrrolidine als tachykinin-antagonisten |
| WO1995007908A1 (en) | 1993-09-17 | 1995-03-23 | Pfizer Inc. | Heteroarylamino and heteroarylsulfonamido substituted 3-benzylaminomethyl piperidines and related compounds |
| US5728830A (en) | 1993-09-22 | 1998-03-17 | Kyowa Hakko Kogyo Co., Ltd. | Farnesyltransferase inhibitor |
| IS4208A (is) | 1993-09-22 | 1995-03-23 | Glaxo Group Limited | 3-(tetrazólýl-benzyl)amínó-piperadidín afleiður |
| IL111235A (en) | 1993-10-15 | 2001-03-19 | Schering Plough Corp | Medicinal preparations for inhibiting protein G activity and for the treatment of malignant diseases, containing tricyclic compounds, some such new compounds and a process for the preparation of some of them |
| DK0723538T3 (da) | 1993-10-15 | 2002-03-18 | Schering Corp | Tricykliske carbamatforbindelser, der er nyttige til inhibition af funktion af G-protein og til behandling af proliferative sygdomme |
| US5661152A (en) | 1993-10-15 | 1997-08-26 | Schering Corporation | Tricyclic sulfonamide compounds useful for inhibition of G-protein function and for treatment of proliferative diseases |
| US5719148A (en) | 1993-10-15 | 1998-02-17 | Schering Corporation | Tricyclic amide and urea compounds useful for inhibition of g-protein function and for treatment of proliferative diseases |
| US5721236A (en) | 1993-10-15 | 1998-02-24 | Schering Corporation | Tricyclic carbamate compounds useful for inhibition of G-protein function and for treatment of proliferative diseases |
| JP2875392B2 (ja) | 1993-10-15 | 1999-03-31 | シェーリング コーポレイション | G−タンパク質機能の阻害および増殖性疾患の治療に有用な三環式スルホンアミド化合物 |
| WO1995011917A1 (en) | 1993-10-25 | 1995-05-04 | Parke, Davis & Company | Substituted tetra- and pentapeptide inhibitors of protein:farnesyl transferase |
| AU7947594A (en) | 1993-10-27 | 1995-05-22 | Merck Sharp & Dohme Limited | Substituted amides as tachykinin antagonists |
| US5344991A (en) | 1993-10-29 | 1994-09-06 | G.D. Searle & Co. | 1,2 diarylcyclopentenyl compounds for the treatment of inflammation |
| DK0677039T3 (da) | 1993-11-04 | 1999-09-27 | Abbott Lab | Cyclobutanderivater som squalen-syntetase- og protein-farnesyltransferaseinhibitorer |
| US5783593A (en) | 1993-11-04 | 1998-07-21 | Abbott Laboratories | Inhibitors of squalene synthetase and protein farnesyltransferase |
| AU681454B2 (en) | 1993-11-05 | 1997-08-28 | Warner-Lambert Company | Substituted DI- and tripeptide inhibitors of protein:farnesyl transferase |
| US6403577B1 (en) | 1993-11-17 | 2002-06-11 | Eli Lilly And Company | Hexamethyleneiminyl tachykinin receptor antagonists |
| US5466823A (en) | 1993-11-30 | 1995-11-14 | G.D. Searle & Co. | Substituted pyrazolyl benzenesulfonamides |
| IT1271462B (it) | 1993-12-03 | 1997-05-28 | Menarini Farma Ind | Antagonisti delle tachichinine,procedimento per la loro preparazione e loro impiego in formulazioni farmaceutiche. |
| US5484799A (en) | 1993-12-09 | 1996-01-16 | Abbott Laboratories | Antifungal dorrigocin derivatives |
| IL111960A (en) | 1993-12-17 | 1999-12-22 | Merck & Co Inc | Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them |
| CA2176130A1 (en) | 1993-12-21 | 1995-06-29 | Thomas Alan Crowell | Non-peptide tachykinin receptor antagonists |
| AU699465B2 (en) | 1993-12-29 | 1998-12-03 | Pfizer Inc. | Diazabicyclic neurokinin antagonists |
| IL112134A (en) | 1993-12-29 | 1999-12-22 | Merck Sharp & Dohme | Substituted morpholine derivatives their preparation and pharmaceutical compositions containing them |
| JPH09507500A (ja) | 1994-01-13 | 1997-07-29 | メルク シヤープ エンド ドーム リミテツド | gem二置換アザシクロ系のタキキニン拮抗薬 |
| EP0741704A1 (en) | 1994-01-28 | 1996-11-13 | MERCK SHARP & DOHME LTD. | Aralkylamino substituted azacyclic therapeutic agents |
| US5393790A (en) | 1994-02-10 | 1995-02-28 | G.D. Searle & Co. | Substituted spiro compounds for the treatment of inflammation |
| GB9402688D0 (en) | 1994-02-11 | 1994-04-06 | Merck Sharp & Dohme | Therapeutic agents |
| US5610165A (en) | 1994-02-17 | 1997-03-11 | Merck & Co., Inc. | N-acylpiperidine tachykinin antagonists |
| IL112778A0 (en) | 1994-03-04 | 1995-05-26 | Merck & Co Inc | Substituted heterocycles, their preparation and pharmaceutical compositions containing them |
| WO1995024612A1 (de) | 1994-03-07 | 1995-09-14 | International Business Machines Corporation | Verfahren und vorrichtung zur schnellen interpolation von zwischenwerten aus periodischen phasenverschobenen signalen und zur erkennung von defekten in einem drehkörper |
| GB9404485D0 (en) | 1994-03-09 | 1994-04-20 | Cancer Res Campaign Tech | Benzamide analogues |
| CN1151156A (zh) | 1994-03-15 | 1997-06-04 | 卫材株式会社 | 异戊二烯基转移酶抑制剂 |
| FR2718136B1 (fr) | 1994-03-29 | 1996-06-21 | Sanofi Sa | Composés aromatiques aminés, procédé pour leur obtention et compositions pharmaceutiques les contenant. |
| RU95104898A (ru) | 1994-03-31 | 1996-12-27 | Бристоль-Мейерз Сквибб Компани (US) | Имидазолсодержащие ингибиторы фарнезид-протеинтрансферазы, способ лечения связанных с ней заболеваний |
| US5523430A (en) | 1994-04-14 | 1996-06-04 | Bristol-Myers Squibb Company | Protein farnesyl transferase inhibitors |
| US5610145A (en) | 1994-04-15 | 1997-03-11 | Warner-Lambert Company | Tachykinin antagonists |
| PE27997A1 (es) | 1994-04-29 | 1997-09-20 | Lilly Co Eli | Antagonistas de receptores de taquicininas |
| AU690682B2 (en) | 1994-05-05 | 1998-04-30 | Merck Sharp & Dohme Limited | Morpholine derivatives and their use as antagonists of tachikinins |
| CN1147260A (zh) | 1994-05-07 | 1997-04-09 | 贝林格尔·英格海姆公司 | 神经激肽(快速激肽)拮抗剂 |
| US5510510A (en) | 1994-05-10 | 1996-04-23 | Bristol-Meyers Squibb Company | Inhibitors of farnesyl protein transferase |
| US5563255A (en) | 1994-05-31 | 1996-10-08 | Isis Pharmaceuticals, Inc. | Antisense oligonucleotide modulation of raf gene expression |
| EE03445B1 (et) | 1994-06-06 | 2001-06-15 | Warner-Lambert Company | Tahükiniini (NK1) retseptori antagonistid |
| EP0686629A3 (en) | 1994-06-10 | 1999-02-10 | Eli Lilly And Company | Cyclohexyl tachykinine receptor antagonists |
| BR9508187A (pt) | 1994-06-10 | 1997-08-12 | Rhone Poulenc Rorer Sa | Produtos e composição farmacêutica |
| US5571792A (en) | 1994-06-30 | 1996-11-05 | Warner-Lambert Company | Histidine and homohistidine derivatives as inhibitors of protein farnesyltransferase |
| CN1067067C (zh) | 1994-07-12 | 2001-06-13 | 伊莱利利公司 | 杂环速激肽受体拮抗物 |
| CA2154116A1 (en) | 1994-07-22 | 1996-01-23 | Philip Arthur Hipskind | 1-aryl-2-acetamidopentanone derivatives for use as tachykinin receptor antagonists |
| GB9415997D0 (en) | 1994-08-08 | 1994-09-28 | Merck Sharp & Dohme | Therapeutic agents |
| GB9415996D0 (en) | 1994-08-08 | 1994-09-28 | Merck Sharp & Dohme | Therapeutic agents |
| WO1996005529A1 (en) | 1994-08-09 | 1996-02-22 | Micron Optics, Inc. | Temperature compensated fiber fabry-perot filters |
| TW432061B (en) | 1994-08-09 | 2001-05-01 | Pfizer Res & Dev | Lactams |
| CA2155448A1 (en) | 1994-08-11 | 1996-02-12 | Katerina Leftheris | Inhibitors of farnesyl protein transferase |
| EP0776884B1 (en) | 1994-08-11 | 2000-01-05 | Banyu Pharmaceutical Co., Ltd. | Substituted amide derivative |
| AU3192495A (en) | 1994-08-12 | 1996-03-07 | Banyu Pharmaceutical Co., Ltd. | N,n-disubstituted amic acid derivative |
| DE69521002T3 (de) | 1994-08-12 | 2010-02-25 | The University Of Utah Research Foundation, Salt Lake City | Mutationen des mit 17q verbundenen Ovarial- und Brustkrebs Empfindlichkeitsgens |
| AU691331B2 (en) | 1994-08-12 | 1998-05-14 | Myriad Genetics, Inc. | Method for diagnosing a predisposition for breast and ovarian cancer |
| AU691327B2 (en) | 1994-08-15 | 1998-05-14 | Merck Sharp & Dohme Limited | Morpholine derivatives and their use as therapeutic agents |
| DE4429506B4 (de) | 1994-08-19 | 2007-09-13 | Degussa Gmbh | Verfahren zur Extraktion natürlicher Carotinoid-Farbstoffe |
| DE4429653C2 (de) | 1994-08-20 | 1997-04-03 | Anton Dr More | Konverter und Verfahren zum Frischen von Metallschmelzen insbesondere von Roheisen zu Stahl |
| WO1996006094A1 (en) | 1994-08-25 | 1996-02-29 | Merrell Pharmaceuticals Inc. | Novel substituted piperidines useful for the treatment of allergic diseases |
| ES2107118T3 (es) | 1994-08-29 | 1997-11-16 | Akzo Nobel Nv | Procedimiento para la preparacion de diesteres cuaternarios. |
| GB9417956D0 (en) | 1994-09-02 | 1994-10-26 | Merck Sharp & Dohme | Therapeutic agents |
| GB9418545D0 (en) | 1994-09-15 | 1994-11-02 | Merck Sharp & Dohme | Therapeutic agents |
| US5457107A (en) | 1994-09-16 | 1995-10-10 | Merck & Co., Inc. | Polymorphic form of a tachykinin receptor antagonist |
| US5935951A (en) | 1994-09-30 | 1999-08-10 | Novartis Finance Corporation | 1-acyl-4-aliphatylaminopiperidine compounds |
| TW397825B (en) | 1994-10-14 | 2000-07-11 | Novartis Ag | Aroyl-piperidine derivatives |
| FR2725986B1 (fr) | 1994-10-21 | 1996-11-29 | Adir | Nouveaux derives de piperidine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| DE69534213T2 (de) | 1994-10-25 | 2006-01-12 | Astrazeneca Ab | Therapeutisch wirksame Heterocyclen |
| GB9421709D0 (en) | 1994-10-27 | 1994-12-14 | Zeneca Ltd | Therapeutic compounds |
| JP4319251B2 (ja) | 1994-11-22 | 2009-08-26 | エヌエックスピー ビー ヴィ | 半導体素子を有し導体トラックが形成されている基板が接着層により結合されている支持本体を有する半導体装置 |
| CA2162786A1 (en) | 1994-11-22 | 1996-05-23 | Philip Arthur Hipskind | Heterocyclic tachykinin receptor antagonists |
| FR2727411B1 (fr) | 1994-11-30 | 1997-01-03 | Rhone Poulenc Rorer Sa | Nouveaux derives de perhydroisoindole, leur preparation et les compositions pharmaceutiques qui les contiennent |
| AU3971295A (en) | 1994-12-09 | 1996-06-26 | Warner-Lambert Company | Substituted tetra- and pentapeptide inhibitors of protein:farnesyl transferase |
| PE38997A1 (es) | 1994-12-13 | 1997-10-02 | Novartis Ag | Antagonista de taquicinina |
| US5589483A (en) | 1994-12-21 | 1996-12-31 | Geron Corporation | Isoquinoline poly (ADP-ribose) polymerase inhibitors to treat skin diseases associated with cellular senescence |
| GB9426103D0 (en) | 1994-12-23 | 1995-02-22 | Merck Sharp & Dohme | Therapeutic agents |
| EP0802953A2 (en) | 1995-01-09 | 1997-10-29 | Magla International Ltd | Wear resistant image printing on latex surfaces |
| ES2229259T3 (es) | 1995-01-12 | 2005-04-16 | Glaxo Group Limited | Derivados de piperidina con actividad antagonista de taquiquinina. |
| JP3929069B2 (ja) | 1995-01-12 | 2007-06-13 | ユニバーシティ オブ ピッツバーグ | プレニルトランスフェラーゼの阻害剤 |
| FR2729390A1 (fr) | 1995-01-18 | 1996-07-19 | Rhone Poulenc Rorer Sa | Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent |
| FR2729951B1 (fr) | 1995-01-30 | 1997-04-18 | Sanofi Sa | Nouveaux composes heterocycliques, procede pour leur preparation et compositions pharmaceutiques en contenant |
| FR2730492B1 (fr) | 1995-02-09 | 1997-03-14 | Rhone Poulenc Rorer Sa | Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent |
| FR2730491B1 (fr) | 1995-02-09 | 1997-03-14 | Rhone Poulenc Rorer Sa | Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent |
| US5633272A (en) | 1995-02-13 | 1997-05-27 | Talley; John J. | Substituted isoxazoles for the treatment of inflammation |
| GB9505491D0 (en) | 1995-03-18 | 1995-05-03 | Merck Sharp & Dohme | Therapeutic agents |
| GB9505492D0 (en) | 1995-03-18 | 1995-05-03 | Merck Sharp & Dohme | Therapeutic agents |
| US5554641A (en) | 1995-03-20 | 1996-09-10 | Horwell; David C. | Nonpeptides as tachykinin antagonists |
| GB9505692D0 (en) | 1995-03-21 | 1995-05-10 | Glaxo Group Ltd | Chemical compounds |
| US5684013A (en) | 1995-03-24 | 1997-11-04 | Schering Corporation | Tricyclic compounds useful for inhibition of g-protein function and for treatment of proliferative diseases |
| NO309272B1 (no) | 1995-03-24 | 2001-01-08 | Takeda Chemical Industries Ltd | Cykliske forbindelser, preparater inneholdende forbindelsene samt mellomprodukter for fremstilling av forbindelsene |
| US5700806A (en) | 1995-03-24 | 1997-12-23 | Schering Corporation | Tricyclic amide and urea compounds useful for inhibition of G-protein function and for treatment of proliferative diseases |
| IL117580A0 (en) | 1995-03-29 | 1996-07-23 | Merck & Co Inc | Inhibitors of farnesyl-protein transferase and pharmaceutical compositions containing them |
| US5565568A (en) | 1995-04-06 | 1996-10-15 | Eli Lilly And Company | 2-acylaminopropanamides as tachykinin receptor antagonists |
| IL117798A (en) | 1995-04-07 | 2001-11-25 | Schering Plough Corp | Tricyclic compounds useful for inhibiting the function of protein - G and for the treatment of malignant diseases, and pharmaceutical preparations containing them |
| US5891872A (en) | 1995-04-07 | 1999-04-06 | Schering Corporation | Tricyclic compounds |
| WO1996031501A1 (en) | 1995-04-07 | 1996-10-10 | Schering Corporation | Carbonyl-piperazinyl and piperidinil compounds which inhibit farnesyl protein transferase |
| US5712280A (en) | 1995-04-07 | 1998-01-27 | Schering Corporation | Tricyclic compounds useful for inhibition of G-protein function and for treatment of proliferative diseases |
| CA2217006C (en) | 1995-04-13 | 2001-05-22 | Hoechst Marion Roussel, Inc. | Novel substituted piperazine derivatives having tachykinin receptor antagonists activity |
| US5831115A (en) | 1995-04-21 | 1998-11-03 | Abbott Laboratories | Inhibitors of squalene synthase and protein farnesyltransferase |
| IL118101A0 (en) | 1995-05-03 | 1996-09-12 | Abbott Lab | Inhibitors of farnesyltransferase |
| JP3071829B2 (ja) | 1995-05-25 | 2000-07-31 | 藤沢薬品工業株式会社 | ニューロキニン受容体拮抗剤としての1−ベンゾイル−2−(インドリル−3−アルキル)−ピペラジン誘導体 |
| WO1997000252A1 (en) | 1995-06-16 | 1997-01-03 | Warner-Lambert Company | Tricyclic inhibitors of protein farnesyltransferase |
| GB9513121D0 (en) | 1995-06-28 | 1995-08-30 | Merck Sharp & Dohme | Therapeutic agents |
| GB9513118D0 (en) | 1995-06-28 | 1995-08-30 | Merck Sharp & Dohme | Therapeutic agents |
| GB9513117D0 (en) | 1995-06-28 | 1995-08-30 | Merck Sharp & Dohme | Therapeutic agents |
| EP0840732B1 (en) | 1995-07-07 | 2001-03-07 | Pfizer Inc. | Substituted benzolactam compounds as substance p antagonists |
| FR2736641B1 (fr) | 1995-07-10 | 1997-08-22 | Rhone Poulenc Rorer Sa | Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent |
| AT402617B (de) | 1995-07-11 | 1997-07-25 | Datacon Schweitzer & Zeindl Gm | Anlage zum automatisierten, hermetischen anlage zum automatisierten, hermetischen verschliessen von gehäusen verschliessen von gehäusen |
| FR2736638B1 (fr) | 1995-07-12 | 1997-08-22 | Rhone Poulenc Rorer Sa | Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent |
| CH690163A5 (fr) | 1995-07-28 | 2000-05-31 | Symphar Sa | Dérivés gem-diphosphonates substitués utiles en tant qu'agents anti-cancers. |
| PT841924E (pt) | 1995-08-02 | 2003-02-28 | Univ Newcastle Ventures Ltd | Compostos de benzimidazolo |
| TW340842B (en) | 1995-08-24 | 1998-09-21 | Pfizer | Substituted benzylaminopiperidine compounds |
| US6020343A (en) | 1995-10-13 | 2000-02-01 | Merck Frosst Canada, Inc. | (Methylsulfonyl)phenyl-2-(5H)-furanones as COX-2 inhibitors |
| JP2002534955A (ja) | 1995-10-18 | 2002-10-15 | メルク エンド カンパニー インコーポレーテッド | シクロペンチルタキキニン受容体アンタゴニスト |
| DE69627377T2 (de) | 1995-11-06 | 2004-02-05 | University Of Pittsburgh | Inhibitoren der protein-isoprenyl-transferase |
| DE19541283A1 (de) | 1995-11-06 | 1997-05-07 | Boehringer Ingelheim Kg | Neue Aminosäurederivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen |
| GB9523244D0 (en) | 1995-11-14 | 1996-01-17 | Merck Sharp & Dohme | Therapeutic agents |
| PT1186606E (pt) | 1995-11-17 | 2004-08-31 | Biotechnolog Forschung Mbh Gbf | Derivados do epotilone sua preparacao e utilizacao |
| WO1997018813A1 (en) | 1995-11-22 | 1997-05-29 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| WO1997019084A1 (en) | 1995-11-23 | 1997-05-29 | Merck Sharp & Dohme Limited | Spiro-piperidine derivatives and their use as tachykinin antagonists |
| GB9524157D0 (en) | 1995-11-25 | 1996-01-24 | Pfizer Ltd | Therapeutic agents |
| RU2135494C1 (ru) | 1995-12-01 | 1999-08-27 | Санкио Компани Лимитед | Гетероциклические соединения и композиция на их основе, проявляющая антагонистическое действие в отношении рецепторов тахикинина |
| IL123568A (en) | 1995-12-08 | 2001-08-08 | Janssen Pharmaceutica Nv | History (Imidazole - 5Il) Methyl-2-quinolinone inhibitors of Prenzyl transferase, their preparation, pharmaceutical preparations containing them and their preparation and drugs containing them |
| GB9525296D0 (en) | 1995-12-11 | 1996-02-07 | Merck Sharp & Dohme | Therapeutic agents |
| CN1326847C (zh) | 1995-12-22 | 2007-07-18 | 先灵公司 | 三环酰胺类用于抑制g-蛋白功能及治疗增生疾病 |
| WO1997026246A1 (en) | 1996-01-16 | 1997-07-24 | Warner-Lambert Company | Substituted histidine inhibitors of protein farnesyltransferase |
| US6673927B2 (en) | 1996-02-16 | 2004-01-06 | Societe De Conseils De Recherches Et D'applications Scientifiques, S.A.S. | Farnesyl transferase inhibitors |
| EP0944388A4 (en) | 1996-04-03 | 2001-08-16 | Merck & Co Inc | INHIBITORS OF FARNESYL PROTEIN TRANSFERASE |
| TR199802049T2 (xx) | 1996-04-12 | 1999-01-18 | G.D.Searle & Co. | COX-2 Inhibit�rlerinin �nilac� olarak s�bstit�e edilmi� benzens�lfonamid t�revleri. |
| NZ332712A (en) | 1996-05-22 | 2000-07-28 | Warner Lambert Co | Polypeptide inhibitors of protein farnesyl transferase |
| EP0918771A4 (en) | 1996-07-15 | 2001-02-07 | Bristol Myers Squibb Co | THIADIOXOBENZODIAZEPINES FOR USE AS FARNESYL PROTEIN TRANSFERASE INHIBITORS |
| US5861419A (en) | 1996-07-18 | 1999-01-19 | Merck Frosst Canad, Inc. | Substituted pyridines as selective cyclooxygenase-2 inhibitors |
| EP1611885A1 (en) | 1996-07-26 | 2006-01-04 | Susan P. Perrine | Use of an inducing agent for the treatment of blood, viral and cellular disorders |
| JP4579351B2 (ja) | 1996-12-03 | 2010-11-10 | スローン−ケッタリング インスティトュート フォア キャンサー リサーチ | エポチロンの合成とその中間体及びその類似物並びにその使用 |
| AU6013998A (en) | 1996-12-30 | 1998-07-31 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| CA2276150A1 (en) | 1996-12-30 | 1998-07-09 | Steven D. Young | Inhibitors of farnesyl-protein transferase |
| WO1999059973A1 (en) | 1998-05-15 | 1999-11-25 | Guilford Pharmaceuticals Inc. | Carboxamide compounds, compositions, and methods for inhibiting parp activity |
| AU1158000A (en) | 1998-10-30 | 2000-05-22 | Lonza A.G. | Method for producing 4- ((2',5'- diamino-6'- halopyrimidine- 4'-YL)amino)- cyclopent- 2-enylmethanols |
| CA2349227C (en) * | 1998-11-03 | 2008-02-05 | Basf Aktiengesellschaft | Substituted 2-phenylbenzimidazoles, the production thereof and their use |
| JP2002529537A (ja) | 1998-11-17 | 2002-09-10 | ビーエーエスエフ アクチェンゲゼルシャフト | 2−フェニルベンズイミダゾールおよび2−フェニルインドール、その製造方法ならびに使用 |
| SK285529B6 (sk) | 1998-11-27 | 2007-03-01 | Basf Aktiengesellschaft | Substituované benzimidazoly, farmaceutická kompozícia s ich obsahom a ich použitie ako inhibítorov PARP |
| EP1151002A4 (en) | 1999-01-29 | 2002-05-02 | Imclone Systems Inc | KDR-SPECIFIC ANTIBODIES AND USES THEREOF |
| GB9904387D0 (en) | 1999-02-25 | 1999-04-21 | Pharmacia & Upjohn Spa | Antitumour synergistic composition |
| EP1187633A4 (en) | 1999-04-08 | 2005-05-11 | Arch Dev Corp | USE OF ANTI-VEGF ANTIBODIES TO ENHANCE RADIATION IN ANTICANCER THERAPY |
| DE19918211A1 (de) | 1999-04-22 | 2000-10-26 | Basf Ag | Cycloalkylsubstituierte Benzimidazole, deren Herstellung und Anwendung |
| DE19920936A1 (de) | 1999-05-07 | 2000-11-09 | Basf Ag | Heterozyklisch substituierte Benzimidazole, deren Herstellung und Anwendung |
| WO2001021615A1 (fr) | 1999-09-17 | 2001-03-29 | Yamanouchi Pharmaceutical Co., Ltd. | Dérivés de benzimidazole |
| US6545004B1 (en) | 1999-10-27 | 2003-04-08 | Cytokinetics, Inc. | Methods and compositions utilizing quinazolinones |
| NZ518480A (en) | 1999-10-27 | 2004-02-27 | Cytokinetics Inc | Methods and compositions utilizing quinazolinones |
| AU2001240542A1 (en) | 2000-02-01 | 2001-08-14 | Basf Aktiengesellschaft | Heterocyclic compounds and their use as parp inhibitors |
| DE10022925A1 (de) | 2000-05-11 | 2001-11-15 | Basf Ag | Substituierte Indole als PARP-Inhibitoren |
| EP1351671A1 (en) | 2001-01-19 | 2003-10-15 | Cytokinetics, Inc. | Triphenylmethane kinesin inhibitors |
| EP1360180A1 (en) | 2001-01-19 | 2003-11-12 | Cytokinetics, Inc. | Phenothiazine kinesin inhibitors |
| WO2002068407A1 (en) | 2001-02-28 | 2002-09-06 | Yamanouchi Pharmaceutical Co., Ltd. | Benzimidazole compound |
| AU2002252614B2 (en) | 2001-04-10 | 2006-09-14 | Merck Sharp & Dohme Corp. | Inhibitors of Akt activity |
| AU2002251266A1 (en) | 2001-04-10 | 2002-10-28 | Merck Sharp And Dohme Limited | Inhibitors of akt activity |
| WO2002083139A1 (en) | 2001-04-10 | 2002-10-24 | Merck & Co., Inc. | Inhibitors of akt activity |
| WO2002083140A1 (en) | 2001-04-10 | 2002-10-24 | Merck & Co., Inc. | Inhibitors of akt activity |
| WO2003007959A1 (en) | 2001-07-16 | 2003-01-30 | Fujisawa Pharmaceutical Co., Ltd. | Quinoxaline derivatives which have parp inhibitory action |
| WO2003013526A1 (en) | 2001-08-08 | 2003-02-20 | Merck & Co. Inc. | Anticoagulant compounds |
| EP1444209A4 (en) | 2001-11-07 | 2005-02-16 | Merck & Co Inc | INHIBITORS OF MITOTIC KINESINS |
| EP1458726B1 (en) | 2001-12-06 | 2009-07-15 | Merck & Co., Inc. | Mitotic kinesin inhibitors |
| AU2002357053B2 (en) | 2001-12-06 | 2008-05-15 | Merck Sharp & Dohme Corp. | Mitotic kinesin inhibitors |
| US7244723B2 (en) | 2001-12-06 | 2007-07-17 | Merck & Co., Inc. | Substituted furopyrimidinones as a mitotic kinesin inhibitors |
| ATE424388T1 (de) | 2001-12-06 | 2009-03-15 | Merck & Co Inc | Mitotische kinesinhemmer |
| EP1481077B1 (en) | 2001-12-06 | 2009-11-04 | Merck & Co., Inc. | Mitotic kinesin inhibitors |
| EP1461359B1 (fr) | 2002-01-18 | 2007-03-21 | Pierre Fabre Medicament | Anticorps anti-igf-ir et leurs applications |
| JPWO2003062234A1 (ja) | 2002-01-23 | 2005-05-19 | 山之内製薬株式会社 | キノキサリン化合物 |
| EP1492487B1 (en) | 2002-03-08 | 2009-11-11 | Merck & Co., Inc. | Mitotic kinesin inhibitors |
| EP1494676B1 (en) | 2002-04-08 | 2013-05-08 | Merck Sharp & Dohme Corp. | Fused quinoxaline derivatives as inhibitors of akt activity |
| CA2481229C (en) | 2002-04-08 | 2010-09-21 | Merck & Co., Inc. | Substituted pyrazine inhibitors of akt |
| JP4451136B2 (ja) | 2002-04-08 | 2010-04-14 | メルク エンド カムパニー インコーポレーテッド | Akt活性阻害薬 |
| WO2003086394A1 (en) | 2002-04-08 | 2003-10-23 | Merck & Co., Inc. | Inhibitors of akt activity |
| JP2006506401A (ja) | 2002-05-23 | 2006-02-23 | メルク エンド カムパニー インコーポレーテッド | 有糸分裂キネシン阻害薬 |
| CA2483627A1 (en) | 2002-05-23 | 2003-12-04 | Merck & Co., Inc. | Mitotic kinesin inhibitors |
| CA2486215A1 (en) | 2002-06-14 | 2003-12-24 | Merck & Co., Inc. | Mitotic kinesin inhibitors |
| IL165624A0 (en) | 2002-06-14 | 2006-01-15 | Merck & Co Inc | Mitotic kinesin inhibitors |
| US20040034078A1 (en) | 2002-06-14 | 2004-02-19 | Agouron Pharmaceuticals, Inc. | Benzimidazole inhibitors of poly(ADP-ribosyl) polymerase |
| JPWO2004014861A1 (ja) | 2002-08-09 | 2005-12-02 | 杏林製薬株式会社 | 4−置換キノリン−8−カルボン酸アミド誘導体とその薬理上許容される付加塩 |
| JP4592587B2 (ja) | 2002-10-18 | 2010-12-01 | メルク・シャープ・エンド・ドーム・コーポレイション | 有糸分裂キネシン阻害剤 |
| JP4590270B2 (ja) | 2002-12-20 | 2010-12-01 | メルク・シャープ・エンド・ドーム・コーポレイション | 有糸分裂キネシン阻害剤 |
| CA2509212A1 (en) | 2002-12-20 | 2004-07-15 | Merck & Co., Inc. | Mitotic kinesin inhibitors |
| JP2006516254A (ja) * | 2003-01-06 | 2006-06-29 | イーライ・リリー・アンド・カンパニー | Pparモジュレータとしての縮合ヘテロ環誘導体 |
| WO2004087050A2 (en) | 2003-03-28 | 2004-10-14 | Merck & Co., Inc. | Mitotic kinesin inhibitors |
| HU0301154D0 (en) | 2003-04-28 | 2003-07-28 | Hideg Kalman Dr | Pharmaceutical composition |
| EP1706386A1 (en) | 2003-12-22 | 2006-10-04 | Eli Lilly And Company | Bicyclic derivatives as ppar modulators |
| KR20060125909A (ko) | 2004-02-26 | 2006-12-06 | 이노텍 파마슈티컬스 코포레이션 | 이소퀴놀린 유도체 및 이의 사용 방법 |
| KR101184036B1 (ko) * | 2004-06-30 | 2012-09-18 | 얀센 파마슈티카 엔.브이. | Parp 저해제로서의 치환 2-알킬 퀴나졸리논 유도체 |
| JP2008510783A (ja) | 2004-08-26 | 2008-04-10 | クドス ファーマシューティカルズ リミテッド | 4−ヘテロアリールメチル置換フタラジノン誘導体 |
| DE602005018506D1 (de) | 2004-09-22 | 2010-02-04 | Pfizer | Verfahren zur herstellung von poly(adp-ribose)polymeraseinhibitoren |
| US7728026B2 (en) | 2005-04-11 | 2010-06-01 | Abbott Laboratories, Inc. | 2-substituted-1 h-benzimidazile-4-carboxamides are PARP inhibitors |
| TWI375673B (en) | 2005-04-11 | 2012-11-01 | Abbott Lab | 1h-benzimidazole-4-carboxamides substituted with a quaternary carbon at the 2-position are potent parp inhibitors |
| CN101316834A (zh) * | 2005-09-29 | 2008-12-03 | 艾博特公司 | 在2位取代有苯基的1h-苯并咪唑-4-甲酰胺是强效parp抑制剂 |
| JP5162465B2 (ja) | 2005-11-15 | 2013-03-13 | アボット・ラボラトリーズ | 置換1h−ベンズイミダゾール−4−カルボキサミド類は強力なparp阻害薬である |
| AU2007232297B2 (en) * | 2006-04-03 | 2012-09-20 | Msd Italia S.R.L. | Amide substituted indazole and benzotriazole derivatives as poly(ADP-ribose)polymerase (PARP) inhibitors |
| ES2385849T3 (es) | 2006-05-02 | 2012-08-01 | Abbott Laboratories | Las 1H-bencimidazol-4-carboxamidas substituidas son potentes inhibidores de la PARP |
| US20090062268A1 (en) * | 2007-08-27 | 2009-03-05 | Lead Therapeutics, Inc. | Novel inhibitors of poly(adp-ribose)polymerase (parp) |
| CN101998959B (zh) * | 2008-02-06 | 2013-08-28 | 生物马林药物股份有限公司 | 聚(adp-核糖)聚合酶(parp)的苯并噁唑甲酰胺抑制剂 |
-
2008
- 2008-01-08 GE GEAP200811413A patent/GEP20115337B/en unknown
- 2008-01-08 RS RS20110236A patent/RS51780B/sr unknown
- 2008-01-08 EP EP08702101A patent/EP2109608B1/en active Active
- 2008-01-08 BR BRPI0806245-5A patent/BRPI0806245B1/pt active IP Right Grant
- 2008-01-08 CA CA2674436A patent/CA2674436C/en active Active
- 2008-01-08 KR KR1020097014520A patent/KR101591656B1/ko active Active
- 2008-01-08 SI SI200832067T patent/SI2805945T1/sl unknown
- 2008-01-08 EP EP11157369.7A patent/EP2336120B1/en active Active
- 2008-01-08 CL CL200800046A patent/CL2008000046A1/es unknown
- 2008-01-08 EA EA200970674A patent/EA016079B1/ru not_active IP Right Cessation
- 2008-01-08 PL PL14176452T patent/PL2805945T3/pl unknown
- 2008-01-08 HR HR20110447T patent/HRP20110447T1/hr unknown
- 2008-01-08 WO PCT/GB2008/050018 patent/WO2008084261A1/en not_active Ceased
- 2008-01-08 PL PL11157369T patent/PL2336120T3/pl unknown
- 2008-01-08 RS RS20190600A patent/RS58936B1/sr unknown
- 2008-01-08 JP JP2009545240A patent/JP4611444B2/ja active Active
- 2008-01-08 PL PL08702101T patent/PL2109608T3/pl unknown
- 2008-01-08 EP EP14176452.2A patent/EP2805945B1/en active Active
- 2008-01-08 US US12/006,993 patent/US8071623B2/en active Active
- 2008-01-08 EP EP19164594.4A patent/EP3536690A1/en active Pending
- 2008-01-08 AR ARP080100061A patent/AR064777A1/es active IP Right Grant
- 2008-01-08 MX MX2009007200A patent/MX2009007200A/es active IP Right Grant
- 2008-01-08 AU AU2008204380A patent/AU2008204380B2/en active Active
- 2008-01-08 DK DK14176452.2T patent/DK2805945T3/da active
-
2009
- 2009-06-09 IL IL199264A patent/IL199264A/en active Protection Beyond IP Right Term
- 2009-07-02 CO CO09068415A patent/CO6210732A2/es active IP Right Grant
- 2009-07-02 DO DO2009000170A patent/DOP2009000170A/es unknown
- 2009-07-02 GT GT200900190A patent/GT200900190A/es unknown
- 2009-07-02 SV SV2009003321A patent/SV2009003321A/es active IP Right Grant
- 2009-07-03 EC EC2009009484A patent/ECSP099484A/es unknown
- 2009-07-03 TN TNP2009000286A patent/TN2009000286A1/fr unknown
- 2009-07-20 MA MA32111A patent/MA31554B1/fr unknown
-
2011
- 2011-06-22 CY CY20111100595T patent/CY1111584T1/el unknown
-
2018
- 2018-04-26 NL NL300937C patent/NL300937I2/nl unknown
- 2018-04-30 LT LTPA2018009C patent/LTC2109608I2/lt unknown
- 2018-05-07 HU HUS1800022C patent/HUS1800022I1/hu unknown
- 2018-05-14 NO NO2018016C patent/NO2018016I2/no unknown
- 2018-05-15 CY CY2018014C patent/CY2018014I1/el unknown
-
2019
- 2019-05-28 HR HRP20190972TT patent/HRP20190972T1/hr unknown
- 2019-07-02 CY CY20191100692T patent/CY1121751T1/el unknown
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2011509252A (ja) * | 2008-01-08 | 2011-03-24 | メルク シャープ エンド ドーム リミテッド | 2−{4−[(3s)−ピペリジン−3−イル]フェニル}−2h−インダゾール−7−カルボキサミドの薬学的に許容される塩 |
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP4611444B2 (ja) | ポリ(adp−リボース)ポリメラーゼ(parp)阻害剤としてのアミド置換インダゾール | |
| JP5989965B2 (ja) | 2−{4−[(3s)−ピペリジン−3−イル]フェニル}−2h−インダゾール−7−カルボキサミドの薬学的に許容される塩 | |
| ES2362214T3 (es) | Indazoles sustituidos con amida como inhibidores de poli(adp-ribosa)polimerasa (parp). | |
| JP2010536842A (ja) | ポリ(adp−リボース)ポリメラーゼ(parp)阻害剤としてのキノリン−4−オン及び4−オキソジヒドロシンノリン誘導体 | |
| HK40006670A (en) | Amide substituted indazoles as poly(adp-ribose)polymerase (parp) inhibitors | |
| HK1154386B (en) | Combinations containing amide substituted indazoles as poly(adp-ribose)polymerase (parp) inhibitors | |
| HK1131137B (en) | Amide substituted indazoles as poly(adp-ribose)polymerase (parp) inhibitors |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20100428 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20100428 |
|
| A871 | Explanation of circumstances concerning accelerated examination |
Free format text: JAPANESE INTERMEDIATE CODE: A871 Effective date: 20100428 |
|
| A975 | Report on accelerated examination |
Free format text: JAPANESE INTERMEDIATE CODE: A971005 Effective date: 20100526 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A132 Effective date: 20100608 |
|
| TRDD | Decision of grant or rejection written | ||
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20101005 |
|
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20101013 |
|
| FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20131022 Year of fee payment: 3 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 4611444 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
| FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20131022 Year of fee payment: 3 |
|
| RD04 | Notification of resignation of power of attorney |
Free format text: JAPANESE INTERMEDIATE CODE: R3D04 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| S111 | Request for change of ownership or part of ownership |
Free format text: JAPANESE INTERMEDIATE CODE: R313113 |
|
| R360 | Written notification for declining of transfer of rights |
Free format text: JAPANESE INTERMEDIATE CODE: R360 |
|
| R370 | Written measure of declining of transfer procedure |
Free format text: JAPANESE INTERMEDIATE CODE: R370 |
|
| S111 | Request for change of ownership or part of ownership |
Free format text: JAPANESE INTERMEDIATE CODE: R313113 |
|
| R350 | Written notification of registration of transfer |
Free format text: JAPANESE INTERMEDIATE CODE: R350 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R153 | Grant of patent term extension |
Free format text: JAPANESE INTERMEDIATE CODE: R153 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R153 | Grant of patent term extension |
Free format text: JAPANESE INTERMEDIATE CODE: R153 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |